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Assay Detail

CHEMBL5035185

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Inhibition of ROS1 (unknown origin) incubated for 120 mins in presence of 33P-ATP
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Proto-oncogene tyrosine-protein kinase ROS (CHEMBL5568)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of the Next-Generation Pan-TRK Kinase Inhibitors for the Treatment of Cancer.
Liu Z, Yu P, Dong L, Wang W, Duan S, Wang B, Gong X, Ye L, Wang H, Tian J.
J Med Chem (2021) 64 : 10286 -10296
PubMed 34253025 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 9.27 9.77

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4298138 REPOTRECTINIB 4.0 1 9.77
CHEMBL5093999 1 9.70
CHEMBL5080010 1 9.00
CHEMBL4297627 SELITRECTINIB 2.0 1 8.94
CHEMBL5070835 1 8.92

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4298138 REPOTRECTINIB IC50 = 0.17 nM 9.77
CHEMBL5093999 IC50 = 0.2 nM 9.70
CHEMBL5080010 IC50 = 1.0 nM 9.00
CHEMBL4297627 SELITRECTINIB IC50 = 1.15 nM 8.94
CHEMBL5070835 IC50 = 1.2 nM 8.92